A-385358 is a potent, selective, cell-permeable Bcl-XL inhibitor with Ki of 0.8 nM, displays >80-fold selectivity over Bcl-2 (Ki=64 nM).
A-385358 shows relatively modest single-agent cytotoxic activity against most tumor cell lines with an EC50 of <500 nM in cells dependent on Bcl-X(L) for survival.
A-385358 enhances the in vitro cytotoxic activity of numerous chemotherapeutic agents; significantly inhibits tumor growth in the A549 xenograft model.
